WO2006112961A2 - Composants a effet synergique augmentant la salivation - Google Patents
Composants a effet synergique augmentant la salivation Download PDFInfo
- Publication number
- WO2006112961A2 WO2006112961A2 PCT/US2006/008016 US2006008016W WO2006112961A2 WO 2006112961 A2 WO2006112961 A2 WO 2006112961A2 US 2006008016 W US2006008016 W US 2006008016W WO 2006112961 A2 WO2006112961 A2 WO 2006112961A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- acid
- food
- salivation
- sanshool
- beverage
- Prior art date
Links
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Classifications
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Definitions
- the present application relates to food or beverage additives that enhance salivation upon consumption of the food or beverage.
- dry mouth (a/k/a, xerostomia) describes an oral condition in which salivary production and/or flow is reduced. Dry mouth may result from one or more of a number of underlying conditions. In many cases, for example, dry mouth occurs due to a natural decrease of saliva production that occurs upon aging. The ability to produce saliva by people in their sixties is typically one-eight of that in young adults. Dry mouth may also affect people with speaking or digestive difficulties or result as a side effect of medication, for example medications used to treat depression and other psychiatric conditions. Dry mouth or xerostomia is also associated with rheumatoid arthritis, diabetes, kidney failure, infection with HIV (the virus that causes AIDS), trauma to the salivary glands, or their ducts or nerves and radiation treatment for mouth or throat cancer.
- HIV the virus that causes AIDS
- a sufficient level of salivation is important for good oral hygiene and taste sensation. Dry mouth is conducive to the growth of microorganisms that cause halitosis or bad breath. Accordingly, many breath freshening products include formulations that increase saliva flow in the oral cavity. Dry mouth decreases taste sensation and, thus, may decrease the ability to taste and enjoy food and beverages. Increased saliva flow, conversely, promotes taste sensation and, thus, may increase the ability to taste and enjoy foods and beverages.
- compositions comprising a) a food acid and ii) a tingling sensate.
- the compositions pleasing have a pleasant taste and promote salivation in products to which they have been added, such as foods, and beverages.
- the tingling sensate is selected from spilanthol, sanshool, hydroxy ⁇ -sanshool, hydroxy ⁇ -sanshool, hydroxy ⁇ -sanshool, sanshool I, sanshool II, sanshoamide, Japanese pepper extract, black pepper extract, chavicine, piperine, echinacea extract, northern prickly ash extract, Nepalese spice timur extract, red pepper oleoresin, 4-(l-menthoxymethyl)-2-phenyl-l,3-dioxolane and jambu oleoresin.
- the tingling sensate is spilanthol that is obtained from jambu oleoresin.
- the food acid is selected from acetic acid, adipic acid, aspartic acid, benzoic acid, caffeotannic acid, citric acid, iso-citric acid, citramalic acid, formic acid, fumaric acid, galacturonic acid, glucuronic acid, glyceric acid, glycolic acid, ketoglutaric acid, ⁇ -ketoglutaric acid, lactic acid, lactoisocitric acid, malic acid, oxalacetic acid, oxalic acid, pyruvic acid, quinic acid, shikimic acid, succinic acid, tannic acid, and tartaric acid.
- the food acids is selected from citric acid, lactic acid, malic acid, succinic acid, fumaric acid, tartaric acid, ascorbic acid or adipic acid.
- the food acid is succinic acid.
- Examples of foods or beverages in which the salivation cocktail may be added include, but are not limited to, carbonated fruit beverages, sport beverages, carbonated cola drinks, wine coolers, cordials, flavored water, powders for drinks, hard candy, soft candy, taffy, chocolates, sugarless candies, chewing gum, bubble gum, condiments, spices and seasonings, dry cereal, oatmeal, granola bars, alcoholic beverages, energy beverages, juices, teas, coffees, salsa, gel beads, film strips for halitosis, gelatin candies, pectin candies, starch candies, lozenges, cough drops, throat lozenges, throat sprays, toothpastes and mouth rinses.
- the present application also provides a method of treating, and a method of inhibiting xerostomia comprising administering a food, beverage, candy, or pharmaceutical dosage form that includes one of the salivation cocktails described in this application to a subject in need thereof.
- the application also provides for the use of a food, beverage, candy, or pharmaceutical dosage form that includes one of the salivation cocktails described in this application to treat or inhibit xerostomia.
- the present application also provides for the use of any of the salivation cocktails described in the this application in the manufacture of a medicament for use in treating or inhibiting xerostomia in a subject.
- a tingling sensate e.g. , spilanthol
- salivation effect of a tingling sensate is synergistically enhanced when it is combined with a food acid. Accordingly, significantly lower amounts of tingling sensate are necessary to achieve a similar or even an increased salivation effect when combined with a food acid.
- common food acids e.g., citric acid, lactic acid, malic acid, succinic acid, fumaric acid, tartaric acid, ascorbic acid and adipic acid
- jambu oleoresin individually, can increase salivation
- the combination of a food acid and a tingling sensate such as spilanthol synergistically increase salivation Due to the synergistic combination, the combined use level of the salivation cocktail can be made lower than would otherwise be predicted if the effects of the food acid and tingling sensate were merely additive.
- the combination In addition to the increased synergistic salivation affect achieved by combining a food acid and a tingling sensate (e.g., spilanthol), the combination also maintains the appealing taste of the food or beverage to which the salivation cocktail is added. This is surprising given that when both of these components are present in a food or beverage alone, the additive usually causes an undesirable off-note or taste (e.g., a food or beverage with green or oily notes). When combined, however, the food acid and tingling sensate do not deteriorate the taste of the food or beverage to which it is added.
- a tingling sensate e.g., spilanthol
- sodium or potassium salts of the food acids when sodium or potassium salts of the food acids are employed, they provide the consumer with a source to replace nutrients lost upon perspiration. Accordingly, the combination of sodium or potassium salts of food acid and tingling sensate (e.g., spilanthol) can be added to a sports hydrating drink or powder or to an energy drink or powder to provide a beverage that will prevent dry mouth, taste good, and replenish nutrients lost upon perspiration.
- tingling sensate e.g., spilanthol
- Food acids can be obtained from nuts, fruits and vegetables, including apples, apricots, avocados, bananas, blackberries, blueberries, boysenberries, cherries, cranberries, currants, figs, gooseberries, grapefruits, grapes, lemons, limes, oranges, peaches, pineapples, plums, strawberries, raspberries, beans, broccoli, carrots, mushrooms, peas, potatoes, rhubarbs, and tomatoes.
- the food acid is an acid that is the principal acid present in the food (e.g., a fruit or vegetable). Food acids are also commercially available (e.g., from. Unilex Exports Ltd., Mumbai, India).
- Examples of food acids that may be used in salivation cocktails include, but are not limited to, acetic, adipic, aspartic, benzoic, caffeotannic acid, citric (including iso-citric), citramalic, formic, fumaric, galacturonic, glucuronic, glyceric, glycolic, ketoglutaric (including ⁇ -ketoglutaric), lactic, lactoisocitric, malic, oxalacetic, oxalic, pyruvic, quinic, shikimic, succinic acid, tannic, and tartaric acids. Additional food acids may be found in the Source Book of Flavors, AVI Publishing Company Inc. (1981), which is hereby incorporated by reference.
- a food acid is at least one of citric, lactic, malic, succinic, fumaric tartaric, ascorbic, or adipic acid.
- the food acid is selected from citric, malic, tartaric and succinic acid.
- the food acid is succinic acid.
- the food acid is not citric and/or malic acid.
- tingling sensates that may be used salivation cocktails include, but are not limited to, spilanthol, sanshool, hydroxy ⁇ -sanshool, hydroxy ⁇ -sanshool, hydroxy ⁇ - sanshool, sanshool I, sanshool II, sanshoamide, piperine, chavicine, 4-(l-menthoxymethyl)-2- phenyl-l,3-dioxolane, effervescing agents and analogs thereof.
- Other tingling sensates can be found in U.S. Pat. No. 5,545,424 which is herein incorporated by reference.
- extracts can also be employed as tingling sensates in accordance with the present application. Oftentimes these extracts contain active ingredients which give the extract itself its tingling character.
- jambu oleoresin extract obtained from a green leafy plant native to Southeast Asia (Spilanthes acmelia, Oleracea) contains spilanthol.
- Other examples of extracts that can employed as tingling sensates include, but are not limited to, Japanese pepper extract (Zanthoxylum peperitum), black pepper extract (Piper nigrum), echinacea extract, northern prickly ash extract, Nepalese spice timur extract, and red pepper oleoresin.
- the tingling sensate is selected from spilanthol, sanshool and ⁇ - hydroxysanshool (timurol).
- the tingling sensate is spilanthol, which is employed via use of jambu oleoresin extract (also referred to as jambu oleoresin). Jambu oleoresin is commercially available from Takasago International Corporation (USA), (Rockleigh New Jersey).
- the tingling sensate is not sanshool, i.e. sanshool is excluded from amongst the list of possible tingling sensates.
- the tingling sensate contains a compound represented by the formula:
- Ri is a branched or unbranched C2-C10 alkenyl group having one or more double bonds which may be conjugated or unconjugated;
- R2 is H or Ci-C ⁇ alkyl
- R3, R4, and R5 are independently H, Ci-Ce alkyl or hydroxy.
- Ri is an unbranched C2-C10 alkenyl group having conjugated double bonds, preferably an unsubstituted C4-C6 alkenyl group having conjugated double bonds
- R- is H
- at least one of R3 or R4 is methyl or hydroxy
- Rs is hydrogen.
- Preferred tingling sensates encompassed by formula B include sanshool, ⁇ -hydroxy sanshool and spilanthol.
- the tingling sensate is represented by the formula:
- Ri is a branched or unbranched C2-C10 alkenyl group having one or more double bonds which may be conjugated or unconjugated;
- R2 is H or Ci-C ⁇ alkyl; and Re is Ci-Cs a branched or unbranched alkyl group, wherein the alkyl group may form a cycloalkyl ring.
- Ri is an unsubstituted C ⁇ -Cio alkenyl group, more preferably a C7-C9 alkenyl group
- R2 is H and RO is a C2-C4 alkyl group.
- R ⁇ is a cyclopropyl group.
- Preferred tingling sensates represented by compound B include N-Isobutyldeca-
- Trans-2-Trans-4-dienamide (pellitorin), n-cyclopropyljtrans-l-cis- ⁇ -nonadienamide, and n- ethyl trans-2-cis-6-nonadienamide.
- compositions of food acids and tingling sensates Compositions of food acids and tingling sensates
- the present invention provides compositions comprising at least one food acid and at least one tingling sensate that are included in a salivation cocktail.
- the salivation cocktail consists essentially of the at least one food acid and the at least one tingling sensate.
- the salivation cocktail is added to a food, beverage, oral personal care product, gum, candy or lozenge.
- the salivation cocktail can contain more than one food acid and/or tingling sensate.
- the components of the salivation cocktail can be combined and then added to the food or beverage, or the components can be added separately to the food or beverage. In either case, the combination of the at least one food acid and the at least one tingling sensate is referred to as the salivation cocktail.
- the salivation cocktail comprises, or consists essentially of, a food acid selected from citric, lactic, malic, succinic, fumaric, tartaric, ascorbic, or adipic acid and a tingling sensate selected from spilanthol, sanshool and ⁇ -hydroxysanshool (timourol).
- the salivation cocktail comprises, or consists essentially of, succinic acid and spilanthol.
- the salivation cocktail comprises, or consists essentially of, succinic acid and jambu oleoresin (which contains spilanthol as its principal active ingredient).
- the salivation cocktail is added to pharmaceutical dosage forms (e.g., a tablet, capsule, drops or lozenges) which contains a medicament.
- pharmaceutical dosage forms e.g., a tablet, capsule, drops or lozenges
- one embodiment of the present invention provides a cough drop or lozenge containing a) menthol or other medicaments for the treatment of sore throat, coughing or other upper respiratory ailments and b) one of the salivation cocktails described in this application.
- a salivation cocktail of the present application is added to a pharmaceutical dosage form which contains an active agent (e.g. an anti-depressant) that typically induces xerostomia as a side effect.
- an active agent e.g. an anti-depressant
- the salivation cocktail is the only medicament included in the composition, and the composition is used to treat or inhibit xerostomia in a subject in need thereof.
- a salivation agent may administered to a subject to alleviate the symptoms of Sjogren's Syndrome, Rheumatoid Arthritis or other condition in which xerostomia is a symptom.
- the salivation cocktail is added to a food, beverage or pharmaceutical dosage form expressly for the purpose of administration to a subject who suffers from xerostomia.
- the salivation cocktail composition is in a form suitable for introduction to a food or beverage for the general public.
- a composition is not in a form suitable for introduction to a food or beverage for the general public when it contains a medicament for the treatment of any physiological condition, ailment and/or disease (except dry mouth), such as decongestants or anorexics (e.g. phenyl propanolamine).
- decongestants or anorexics e.g. phenyl propanolamine
- any of the aforementioned tingling sensates e.g. spilanthol or sanshool
- food acids eg.
- citric acid singularly or combined, are not considered a medicament since the general public is presumed to have relatively normal salivation levels, and the salivation cocktail is added to supplement these normal levels of salivation for hedonistic purposes (e.g., to make food taste better).
- a composition is also not in a form suitable for introduction to a food or beverage for the general public when it contains exotic ingredients such as powder from liver, lungs, heart, kidneys, spleen or other organs, since the inclusion of these components in foods or beverages would not be hedonistically appealing to the general public.
- the compositions disclosed in U.S. Patent No. 4,639,368 and Japanese Publication No. 57-118518 are compositions that are not in a form suitable for introduction to a food or beverage for the general public.
- compositions include all the compositions disclosed in the present application, except that all the compositions disclosed in U.S. Patent No. 4,639,368 and Japanese Publication No. 57-118518 are excluded. These patents and applications are hereby incorporated by reference.
- Use levels of the salivation cocktail may range from about 0.01 % or 0.1 % to about 1 % or 5% , or from about 0.05% or 0.1 % to about 0.3% or 1 % , or from about 0.035% or 0.07% to about 0.125% or 0.25% , or from about 0.1 % to about 0.2% based on the total weight of the food or beverage.
- the use level of salivation cocktail is about 0.12% .
- the above percentages are by volume of the salivation cocktail, based on the total volume of the beverage batch (v/v).
- For foods, the above percentages are by volume of the salivation cocktail, based on the total weight of the food batch (v/w).
- the volume ratio of food acid to tingling sensate in the salivation cocktail may range from about 100:1 or 50:1 to about 1:50 or 1:100 or from about 50:1 or 25:1 to about 5:1 or 1:1. In one embodiment, the volume ratio of food acid to tingling sensate ranges from about 7:1 or 11:1 to about 12:1 or 15:1. In one embodiment, the ratio of food acid to tingling sensate is about 11.7:1. In the above ratios, the amount of tingling sensate refers to the volume of the active ingredient, not the volume of extract (e.g., jambu oleoresin) from which the active ingredient (e.g., spilanthol) is obtained.
- extract e.g., jambu oleoresin
- the salivation cocktails described above can be added to, for example, compositions for the preparation of carbonated fruit beverages, carbonated cola drinks, wine coolers, cordials, flavored water, powders for drinks (e.g., powdered sports or "hydrating” drinks), hard candy, soft candy, taffy, chocolates, sugarless candies, chewing gum, bubble gum, condiments, spices and seasonings, dry cereal, oatmeal, granola bars, alcoholic beverages, energy beverages, juices, teas, coffees, salsa, gel beads, film strips for halitosis, gelatin candies, pectin candies, starch candies, lozenges, cough drops, throat lozenges, throat sprays, toothpastes and mouth rinses.
- powders for drinks e.g., powdered sports or "hydrating” drinks
- hard candy soft candy
- taffy chocolates
- sugarless candies chewing gum
- condiments, spices and seasonings dry cereal
- oatmeal granola bars
- alcoholic beverages energy beverages
- salivation cocktails and relative amounts of food acids and tingling sensates can be adjusted by persons of ordinary skill in the art depending of the flavor of the additives employed in the end use food or beverage, or the taste or flavor of the end product itself.
- chewing gum and bubble gum are excluded from the possible foods or beverages which the salivation agent may be added.
- a carbonated citrus beverage may be prepared with the ingredients shown below:
- the Salivation Cocktail has the following composition:
- a Diet Cola Carbonated Beverage may be prepared with the ingredients shown below:
- This syrup may be used to make 3L of a finished beverage.
- a cranberry apple flavored still beverage containing 3 % Juice may be prepared from the ingredients shown below:
- a lO Proof Carbonated Cooler [Plum Type Flavor] may be prepared from the ingredients shown below:
- This syrup may be used to make 3L of finished product
- a 35 Proof Cordial [Raspberry Type Flavor] may be prepared from the ingredients shown below:
- a 60 Proof Cordial [41] A 60 Proof Cordial [Cherry Type Flavor] may be prepared from the ingredients shown below:
- a flavored water (Nat. Sweetened) [Strawberry Flavor Type] may be prepared from the ingredients shown below:
- a flavored water (Sweetened w/Sucralose) [Lemon Strawberry Type] may be prepared from the ingredients shown below:
- a powdered hydrating mix may be prepared from the ingredients shown below:
- a hard candy may be prepared from the ingredients shown below:
- a sugarless candy formula may be prepared from the ingredients shown below:
- a chewing gum may be prepared from the ingredients shown below:
- the first batch (Batch A) contained 0.5% (by volume of grapefruit flavor.
- the second, third, and fourth batches of grapefruit mint hard candy also contained 0.5% by volume of grapefruit flavor.
- the second batch (Batch B) contained 0.65% by volume of salivation cocktail set forth below in which jambu oleoresin is the only salivation component:
- the third batch (Batch C) contained a salivation cocktail shown below in which succinic acid is the only salivation component:
- the third batch (Batch D) contained a salivation cocktail described in Example 1 containing a synergistic combination of succinic acid and spilanthol obtained from jambu oleoresin.
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Abstract
L'invention concerne une préparation augmentant la salivation, comprenant un acide alimentaire et un agent provoquant une sensation de picotement. L'association de l'acide alimentaire et de l'agent provoquant une sensation de picotement a un effet synergique qui augmente la salivation.
Priority Applications (1)
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EP06769774.8A EP1863466B1 (fr) | 2005-03-03 | 2006-03-03 | Composants a effet synergique augmentant la salivation |
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US59400405P | 2005-03-03 | 2005-03-03 | |
US60/594,004 | 2005-03-03 |
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WO2006112961A3 WO2006112961A3 (fr) | 2007-01-25 |
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US (2) | US8435542B2 (fr) |
EP (1) | EP1863466B1 (fr) |
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
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EP2031977A2 (fr) * | 2006-06-12 | 2009-03-11 | Firmenich S.A. | Composition favorisant la génération de salive et provoquant un effet de fourmiement dans la bouche |
WO2015036656A3 (fr) * | 2013-09-13 | 2015-05-14 | Replicon Health Oy | Procédé d'amélioration de la production d'énergie et du métabolisme dans des cellules |
US10500176B2 (en) | 2013-09-13 | 2019-12-10 | Replicon Health Oy | Method for enhancing energy production and metabolism in cells |
US11357746B2 (en) | 2013-09-13 | 2022-06-14 | Replicon Health Oy | Method for enhancing energy production and metabolism in cells |
US20210177800A1 (en) * | 2017-09-08 | 2021-06-17 | Scicann Therapeutics Inc. | Compositions comprising a cannabinoid and spilanthol |
Also Published As
Publication number | Publication date |
---|---|
WO2006112961A3 (fr) | 2007-01-25 |
US20060204551A1 (en) | 2006-09-14 |
EP1863466A2 (fr) | 2007-12-12 |
US9814748B2 (en) | 2017-11-14 |
US20140099391A1 (en) | 2014-04-10 |
EP1863466B1 (fr) | 2017-08-09 |
US8435542B2 (en) | 2013-05-07 |
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